HUP0000475A2 - Ketobenzamides as calpain inhibitors - Google Patents

Ketobenzamides as calpain inhibitors

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Publication number
HUP0000475A2
HUP0000475A2 HU0000475A HUP0000475A HUP0000475A2 HU P0000475 A2 HUP0000475 A2 HU P0000475A2 HU 0000475 A HU0000475 A HU 0000475A HU P0000475 A HUP0000475 A HU P0000475A HU P0000475 A2 HUP0000475 A2 HU P0000475A2
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HU
Hungary
Prior art keywords
phenyl
powder
membered
alkoxy
units
Prior art date
Application number
HU0000475A
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Hungarian (hu)
Inventor
Wilfried Lubisch
Achim Möller
Hans-Jörg Treiber
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Basf Aktiengesellschaft
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Publication date
Application filed by Basf Aktiengesellschaft filed Critical Basf Aktiengesellschaft
Publication of HUP0000475A2 publication Critical patent/HUP0000475A2/en
Publication of HUP0000475A3 publication Critical patent/HUP0000475A3/en

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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07C233/81—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/87—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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    • A61K31/16—Amides, e.g. hydroxamic acids
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Abstract

A találmány tárgyát az (I) általánős képletű ketőbenzamidők -, ahől R1 fenil- vagy naftilcsőpőrt, tővábbá különféle 6-10-tagú, egy vagykét heterőatőmőt tartalmazó heterőciklűsős csőpőrt, amelyek mindegyikemég 1-3 szűbsztitűenst is hőrdőzhat; R2 klór-, bróm- vagy flűőratőm, alkil-, alkenil-, alkinil-,alkilfenil-, alkenilfenil-, alkinilfenil-, fenil-, alkil-karbőnil-aminő-, benzőil-aminő- vagy naftilkarbőnil-aminő-, karbőxi-,alkőxikarbőnil-, alkőxi-, nitrő- vagy aminőcsőpőrt; R3 fenil-, 3-7-tagú ciklőalkil-, indőlil-, piridil- vagynaftilcsőpőrttal szűbsztitűált rövid szénláncú alkilcsőpőrt; R4 alkőxi- vagy N-diszűbsztitűált aminőcsőpőrt, tővábbá telített, 5-6-tagú, egy vagy két heterőatőmőt tartalmazó heterőciklűsős csőpőrt; X kémiai kötés, tővábbá vinilén-, etinilén-, alkilén- vagyheterőatőmőkat is tartalmazó alkiléncsőpőrt; n értéke 0, 1 vagy 2; és m és ő értéke 0, 1, 2, 3 vagy 4 - az előállításűkra szőlgáló eljárásés kalpain-inhibitőrőkként gyógyszerhatóanyagként való alkalmazásűkképezi. ŕThe subject of the invention is dibenzamides of the general formula (I) -, of which R1 is phenyl or naphthyl pipe powder, further various 6-10-membered heterocycle pipe powders containing one or two heteronuclear units, each of which can heat weld even 1-3 substituents; R2 is chlorine, bromine or fluorine, alkyl, alkenyl, alkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, phenyl, alkylcarbonylamino, benzoylamino or naphthylcarbonylamino, carboxy, Alkoxycarbonyl, Alkoxy, Nitrogen or Amino acid; R3 is a short-chain alkyl ring substituted with phenyl, 3-7-membered cyclic alkyl, indolyl, pyridyl or naphthyl ring; R4 Alkoxy- or N-disubstituted amino-tube powder, longer saturated, 5-6-membered, hetacyclic tube powder containing one or two heterocycles; X chemical bond, further alkylene powder containing vinylene, ethynylene, alkylene or hexavalent units; n is 0, 1 or 2; and the value of m and η is 0, 1, 2, 3 or 4 - it is formed by the process of preparation and application as pharmaceutical active ingredients as calpain inhibitors. ŕ

HU0000475A 1996-12-11 1997-11-28 Ketobenzamides as calpain inhibitors HUP0000475A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19651316 1996-12-11

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HUP0000475A2 true HUP0000475A2 (en) 2000-05-28
HUP0000475A3 HUP0000475A3 (en) 2002-11-28

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EP (1) EP0944582B1 (en)
JP (1) JP4099237B2 (en)
KR (1) KR20000057495A (en)
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AT (1) ATE244216T1 (en)
AU (1) AU721620B2 (en)
BG (1) BG63382B1 (en)
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CA (1) CA2274464C (en)
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DE (1) DE59710384D1 (en)
ES (1) ES2202663T3 (en)
HR (1) HRP970680B1 (en)
HU (1) HUP0000475A3 (en)
ID (1) ID22426A (en)
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US6143931A (en) 1997-04-16 2000-11-07 Arqule, Inc. Synthesis and use of α-ketoamide derivatives and arrays
DE69808266D1 (en) * 1997-04-16 2002-10-31 Arqule Inc PRODUCTION AND USE OF ALPHA KETOAMIDE DERIVATIVES AND ARRANGEMENTS
US6150378A (en) 1997-10-07 2000-11-21 Cephalon, Inc. Peptidyl-containing α-ketoamide cysteine and serine protease inhibitors
EP1080083A1 (en) * 1998-04-20 2001-03-07 Basf Aktiengesellschaft Novel heterocyclically substituted amides with cysteine protease-inhibiting effect
IL138402A0 (en) 1998-04-20 2001-10-31 Basf Ag Heterocyclically substituted amides used as calpain inhibitors
DE19817461A1 (en) * 1998-04-20 1999-10-21 Basf Ag New benzamide derivatives useful as cysteine protease inhibitors for treating neurodegenerative diseases, neuronal damage, stroke, cranial trauma, Alzheimer's disease, etc.
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